Identification and Characterization of Small Molecule Inhibitors of a Class I Histone Deacetylase from Plasmodium falciparum
Barker, Robert H.
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CitationPatel, Vishal, Ralph Mazitschek, Bradley Coleman, Cokey Nguyen, Sameer Urgaonkar, Joseph Cortese, Robert H. Barker, et al. 2009. Identification and characterization of small molecule inhibitors of class I Histone deacetylase from Plasmodium falciparum. Journal of Medicinal Chemistry 52:2185-2187.
AbstractA library of approximately 2000 small molecules biased toward inhibition of histone deacetylases was assayed for antimalarial activity in a high-throughput P. falciparum viability assay. Active compounds were cross-analyzed for induction of histone hyperacetylation in a human myeloma cell line to identify HDAC inhibitors with selectivity for P. falciparum over the human host. To verify on-target selectivity, pfHDAC-1 was expressed and purified and a biochemical assay for pfHDAC-1 activity was established.
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